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Assay Detail

CHEMBL1218399

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Displacement of [3H]IP3 from full-length rat recombinant IP3R1 expressed in chicken DT40 cells by equilibrium competitive binding assay
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Cell Type DT40
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Inositol 1,4,5-trisphosphate-gated calcium channel ITPR1 (CHEMBL2804)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Synthetic partial agonists reveal key steps in IP3 receptor activation.
Rossi AM, Riley AM, Tovey SC, Rahman T, Dellis O, Taylor EJ, Veresov VG, Potter BV, Taylor CW.
Nat Chem Biol (2009) 5 : 631 -639
PubMed 19668195 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 11 8.47 9.35

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1213158 1 9.35
CHEMBL1213159 1 9.07
CHEMBL1212943 1 9.05
CHEMBL1213160 1 9.05
CHEMBL204385 ADENOPHOSTIN A 1 8.90
CHEMBL1213163 1 8.12
CHEMBL1213161 1 8.11
CHEMBL279107 INS(1,4,5)P3 1 7.90
CHEMBL1213201 1 7.77
CHEMBL1213202 1 7.36
CHEMBL1213162 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1213158 Kd = 0.45 nM 9.35
CHEMBL1213159 Kd = 0.86 nM 9.07
CHEMBL1212943 Kd = 0.9 nM 9.05
CHEMBL1213160 Kd = 0.89 nM 9.05
CHEMBL204385 ADENOPHOSTIN A Kd = 1.26 nM 8.90
CHEMBL1213163 Kd = 7.62 nM 8.12
CHEMBL1213161 Kd = 7.82 nM 8.11
CHEMBL279107 INS(1,4,5)P3 Kd = 12.5 nM 7.90
CHEMBL1213201 Kd = 17.1 nM 7.77
CHEMBL1213202 Kd = 43.6 nM 7.36
CHEMBL1213162 Kd - -